IndraLab

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"To directly examine whether TPCA-1 inhibits phosphorylation of STAT1 and STAT2 via inhibition of JAK1, we performed an in situ kinase activity assay using a purified recombinant human JAK1 in the presence of TPCA-1, ruxolitinib or BMS-345541 ( xref ). ruxolitinib and TPCA-1 were able to inhibit JAK1 kinase activity in a dose dependent manner with an IC 50 of 4.33 nM and 43.78 nM, respectively, while BMS-345541 did not affect the kinase enzymatic activity."
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"Moreover, using an in situ kinase assay, we demonstrated that TPCA-1 can directly inhibit JAK1 kinase activity [XREF_BIBR]."
| PMC
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"These data provide biochemical evidence that TPCA-1 directly inhibits JAK1 kinase, which can explain inhibition of STAT1 and STAT2 phosphorylation in vitro ( xref )."
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"Moreover, an in situ kinase assay provided biochemical evidence that TPCA-1 directly inhibits JAK1 kinase activity."
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"These data provide biochemical evidence that TPCA-1 directly inhibits JAK1 kinase, which can explain inhibition of STAT1 and STAT2 phosphorylation in vitro (XREF_FIG)."
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"ruxolitinib and TPCA-1 were able to inhibit JAK1 kinase activity in a dose dependent manner with an IC 50 of 4.33 nM and 43.78 nM, respectively, while BMS-345541 did not affect the kinase enzymatic activity."
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